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IDEAYA Licenses Phase 1 Compound LXS196 For The Treatment Of Cancers With GNAQ And GNA11 Mutations

SOUTH SAN FRANCISCO, Calif., Oct. 23, 2018 /PRNewswire/ -- IDEAYA Biosciences, Inc., has entered into an exclusive license agreement with Novartis to develop and commercialize Novartis' LXS196, a Phase 1 protein kinase C (PKC) inhibitor for the treatment of cancers with GNAQ and GNA11 mutations.

LXS196, which will be recoded as IDE196 by IDEAYA for future development, is a potent small molecule inhibitor of PKC demonstrating early clinical activity and tolerability in an ongoing Phase 1 study of IDE196 for patients with metastatic uveal melanoma (MUM). IDE196 is active across multiple PKC isoforms and is highly selective relative to other kinases.  MUM is an orphan disease of high unmet medical need, with median overall survival of approximately 10 months and no FDA approved therapies. 

"There are no approved therapies for metastatic uveal melanoma, and continued development of promising clinical stage agents, such as IDE196, with a clear genetic biomarker rationale to treat patients that harbor GNAQ and GNA11 mutations through PKC are paramount," said Dr. Sophie Piperno‐Neumann, M.D., LXS196 Study Investigator and Medical Oncologist at Institute Curie, Paris, France.

IDEAYA will continue development in metastatic uveal melanoma and will also explore a tumor agnostic basket study of solid tumors with mutations of GNAQ and GNA11. Both GNAQ and GNA11 mutations are listed in multiple diagnostic panels, including the FoundationOne CDx™ NGS panel, FoundationOne™Liquid Biopsy Panel, and the Guardant360® Liquid Biopsy panel, which provides a clear path towards identifying patients. IDEAYA is also evaluating the potential use of IDE196 to target various PKC fusion isoforms.

Novartis is conducting an ongoing Ph1 clinical trial, entitled "A Phase I, multi-center, open-label, study of LXS196, an oral protein kinase C inhibitor, in patients with metastatic uveal melanoma" ( Identifier: NCT02601378). In the ongoing trial, IDE196 is being studied as a single-agent and in combination therapy with HDM201, Novartis' human double minute 2 (HDM2) inhibitor, an important negative regulator of the p53 tumor suppressor.  Notably, approximately 90% of metastatic uveal melanoma patients harbor activating mutations in GNA11 or GNAQ. 

"Targeting PKC, a pathway which is active in this disease, may result in improved clinical outcomes, and the data with IDE196 treatment thus far demonstrate objective responses, with tolerability that will enable ongoing and future monotherapy and combination trials," said Dr. Ellen Kapiteijn, M.D. Ph.D., LXS196 Study Investigator and Medical Oncologist at Leiden University Medical Center, Leiden, Netherlands.

Under the exclusive license, Novartis increased its equity ownership in IDEAYA, and is due future milestones and royalties, and Novartis will continue the ongoing IDE196 monotherapy and combination study with the Novartis HDM201 compound.  IDEAYA has exclusive rights for further clinical development of IDE196, together with unrestricted rights to commercialize worldwide. 

"IDE196 enhances our robust precision medicine pipeline, and we are ecstatic to develop this first-in-class therapy for cancer patients who harbor activating mutations of GNAQ and GNA11," said Yujiro Hata, Chief Executive Officer of IDEAYA. "Novartis has been an investor in IDEAYA since the Series A, so we are pleased to enter into this agreement and further enhance our strategic relationship."

About IDEAYA Biosciences

IDEAYA is an oncology-focused precision medicine company committed to the discovery and development of innovative synthetic lethality, targeted and immuno-oncology medicines for biomarker-defined cancer populations.  IDEAYA, located in South San Francisco and San Diego, California, has assembled leading scientists, clinicians, and advisors with extensive knowledge and expertise in cancer biology, immunology, small molecule chemistry, biomarker discovery, and clinical development. For more information, please visit

Investor and Media Contact:
IDEAYA Biosciences
Paul Stone
SVP, General Counsel and Head of Operations

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